Usage
Escitalopram Oxalate is prescribed for the acute and maintenance treatment of Major Depressive Disorder (MDD) in adults and adolescents (12-17 years old), and the acute treatment of Generalized Anxiety Disorder (GAD) in adults. It is also sometimes used off-label for obsessive-compulsive disorder, insomnia, and vasomotor symptoms associated with menopause.
It’s pharmacological classification is antidepressant, specifically a Selective Serotonin Reuptake Inhibitor (SSRI).
Escitalopram increases the extracellular level of the neurotransmitter serotonin by inhibiting its reuptake into presynaptic neurons. This enhances serotonergic activity in the central nervous system.
Alternate Names
Generic Name: Escitalopram
Brand Names: Lexapro, Cipralex
How It Works
Pharmacodynamics: Escitalopram selectively inhibits the reuptake of serotonin, increasing its concentration in the synaptic cleft and thus enhancing serotonergic neurotransmission. It has minimal effects on norepinephrine and dopamine reuptake.
Pharmacokinetics:
- Absorption: Escitalopram is well-absorbed orally, and food does not significantly affect its bioavailability.
- Metabolism: Primarily metabolized in the liver by CYP2C19, with contributions from CYP3A4 and CYP2D6. Genetic polymorphisms in these enzymes can affect drug levels.
- Elimination: Excreted primarily in urine (8-10% unchanged), with a small amount in feces. The elimination half-life is approximately 27-32 hours, which allows for once-daily dosing.
Mode of Action: Escitalopram binds to the serotonin transporter (SERT) on the presynaptic neuron, blocking the reuptake of serotonin. This leads to increased serotonin levels in the synapse.
Receptor Binding/Enzyme Inhibition: Escitalopram is a potent and selective SERT inhibitor. It has weak affinity for other receptors, including dopamine and norepinephrine transporters.
Elimination Pathways: Primarily renal excretion (as metabolites and a small amount of unchanged drug), with minor hepatic elimination.
Dosage
Standard Dosage
Adults:
- MDD and GAD: Initial dose: 10 mg orally once daily, taken in the morning or evening. The dose may be increased to a maximum of 20 mg/day after at least one week if needed.
Children (12-17 years):
- MDD: Initial dose: 10 mg orally once daily. The dose may be increased to a maximum of 20 mg/day after at least three weeks, if needed.
Special Cases:
- Elderly Patients: 10 mg once daily is generally recommended due to potential for age-related changes in metabolism and increased sensitivity to side effects.
- Patients with Renal Impairment: No dosage adjustment is needed for mild to moderate renal impairment. Use with caution in severe renal impairment (creatinine clearance < 30 mL/min).
- Patients with Hepatic Dysfunction: 10 mg once daily is recommended due to slower metabolism.
- Patients with Comorbid Conditions: Careful assessment and dosage adjustments may be required depending on the specific comorbid conditions.
Clinical Use Cases
Escitalopram is not typically indicated for use in the clinical settings of intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations like status epilepticus or cardiac arrest.
Dosage Adjustments
Dose adjustments might be necessary based on individual patient response, tolerability, and the presence of renal or hepatic impairment. Genetic polymorphisms affecting CYP2C19 metabolism should be considered, with a lower starting dose and slower titration for poor metabolizers.
Side Effects
Common Side Effects:
Nausea, insomnia, somnolence, dizziness, increased sweating, constipation, fatigue, dry mouth, decreased libido, and anorgasmia.
Rare but Serious Side Effects:
Serotonin syndrome (fever, muscle rigidity, confusion, seizures), hyponatremia (low sodium), bleeding disorders, suicidal thoughts/behavior (particularly in young adults), mania/hypomania, and angle-closure glaucoma.
Long-Term Effects:
Potential long-term effects include sexual dysfunction, weight gain, and withdrawal symptoms upon discontinuation.
Adverse Drug Reactions (ADR):
Clinically significant ADRs include serotonin syndrome, hyponatremia, and QTc prolongation (rarely).
Contraindications
- Concurrent or recent (within 14 days) use of MAOIs.
- Hypersensitivity to escitalopram or citalopram.
Drug Interactions
Escitalopram interacts with:
- MAOIs: Concurrent use is contraindicated due to risk of serotonin syndrome.
- CYP2C19 inhibitors (e.g., cimetidine): May increase escitalopram levels.
- CYP3A4 inhibitors (e.g., ketoconazole): May increase escitalopram levels.
- Serotonergic drugs (e.g., triptans, tramadol): Increased risk of serotonin syndrome.
- NSAIDs, anticoagulants: Increased bleeding risk.
- Alcohol: May potentiate sedative effects.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C. Use only if the potential benefit outweighs the potential risk to the fetus.
- Breastfeeding: Escitalopram is excreted in breast milk. Weigh the risks and benefits carefully, considering the infant’s potential exposure.
Drug Profile Summary
- Mechanism of Action: SSRI, inhibits serotonin reuptake.
- Side Effects: Nausea, insomnia, sexual dysfunction, dizziness, sweating, constipation, fatigue. Serious side effects include serotonin syndrome, hyponatremia, bleeding, and suicidal ideation.
- Contraindications: Concurrent MAOI use, hypersensitivity.
- Drug Interactions: MAOIs, CYP2C19/3A4 inhibitors, serotonergic drugs, NSAIDs, alcohol.
- Pregnancy & Breastfeeding: Category C; excreted in breast milk. Use with caution.
- Dosage: MDD/GAD (adults): 10-20 mg/day; MDD (adolescents): 10-20 mg/day; Elderly/Hepatic impairment: 10 mg/day.
- Monitoring Parameters: Monitor for mood changes, suicidal ideation, hyponatremia, and serotonin syndrome.
Popular Combinations
Escitalopram is sometimes combined with other psychotropic medications, such as mood stabilizers or other antidepressants, depending on the patient’s specific condition and needs. This should be done under the guidance of a psychiatrist experienced in combination therapy.
Precautions
- General Precautions: Screen for bipolar disorder, suicidality, and bleeding risk.
- Specific Populations: Monitor elderly patients for hyponatremia and other side effects. In adolescents and young adults, closely monitor for suicidal ideation.
- Lifestyle Considerations: Advise patients about potential sedative effects and caution against alcohol use.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Escitalopram Oxalate?
A: Adults: 10-20 mg once daily for MDD and GAD. Adolescents (12-17 years): 10-20 mg once daily for MDD. Elderly/Hepatic impairment: Start with 10 mg once daily.
Q2: How long does it take for Escitalopram to work?
A: It can take 2-4 weeks, or even longer, to experience significant improvement in symptoms.
Q3: What are the most common side effects of Escitalopram?
A: Nausea, insomnia, sexual dysfunction, dizziness, increased sweating, and constipation.
Q4: Can Escitalopram be used during pregnancy?
A: Pregnancy Category C. Use only if the potential benefit outweighs the potential risk to the fetus. Closely monitor pregnant patients.
Q5: Is Escitalopram addictive?
A: Escitalopram is not considered physically addictive, but withdrawal symptoms can occur upon abrupt discontinuation. Therefore, a gradual taper is recommended.
Q6: Can Escitalopram be taken with other medications?
A: It can interact with several medications, such as MAOIs, CYP inhibitors, and serotonergic drugs. Always review a patient’s medication list for potential interactions.
Q7: What should I do if a patient experiences suicidal thoughts while taking Escitalopram?
A: Immediately assess the patient’s risk and consider hospitalization if necessary. Re-evaluate the treatment plan and potentially discontinue escitalopram.
Q8: How should Escitalopram be discontinued?
A: Gradually taper the dose to minimize withdrawal symptoms. The rate of tapering should be individualized based on patient tolerance.
Q9: What are the symptoms of serotonin syndrome?
A: Agitation, confusion, rapid heart rate, high blood pressure, muscle rigidity, tremors, sweating, diarrhea, and fever. Severe cases can lead to seizures, coma, and death.
Q10: Are there any specific monitoring parameters for patients on Escitalopram?
A: Monitor for changes in mood, suicidal ideation, development of serotonin syndrome, hyponatremia, and any unusual bleeding. Regularly evaluate the patient’s response to treatment.
